Bayer Intellectual Property Gmbh

Zentaris Ag

Hans Peter Muhn

Ulrich Klar

Rolf Bohlmann

Thomas Frenzel

Joachim Kuhnke

Sven Ring

Marcus Koppitz

Kenneth Jay Shaw

Frederik Menges

Klaus Paulini

Steffen Borden

Katja Prelle

Jan Hübner

Holger Hess-Stump

The invention relates to 17-(1'-propenyl)-17-3&#x2032;-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R, R, R, R, R, R, Rand Rhave the meanings stated in Claim, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action. 

17-(1'propenyl)-17-3&#x2032;-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative

This invention provides new tetrahydrocarbazole derivatives that act as ligands for G-protein-coupled receptors (GPCR), especially as antagonists of the gonadotropin-releasing hormone (GnRH). A pharmaceutical composition that contains these new tetrahydrocarbazole derivatives as well as a process for the production of the new tetrahydrocarbazole derivatives are also provided. Moreover, this invention relates to the administration of tetrahydrocarbazole derivatives for treating pathologic conditions that are mediated by GPCR, especially for inhibiting GnRH, in mammals, especially humans, who require such an administration, as well as the use of tetrahydrocarbazole derivatives for the production of a pharmaceutical agent for treating GPCR-mediated pathologic conditions, especially for inhibiting GnRH.

Tetrahydrocarbazol derivatives as ligands for G-protein-coupled receptors (GPCR)

Growing community of inventors

Berlin, Germany

Hans Peter Muhn